E3263
依法克生 盐酸盐
≥98% (HPLC)
别名:
2-Ethyl-2-(imidazolin-2-yl)-2,3-dihydrobenzofuran hydrochloride, RX 821037A
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关于此项目
经验公式（希尔记法）:
C13H16N2O · HCl
化学文摘社编号:
分子量:
252.74
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
质量水平
方案
≥98% (HPLC)
溶解性
H2O: >20 mg/mL
SMILES字符串
Cl.CCC1(Cc2ccccc2O1)C3=NCCN3
InChI
1S/C13H16N2O.ClH/c1-2-13(12-14-7-8-15-12)9-10-5-3-4-6-11(10)16-13;/h3-6H,2,7-9H2,1H3,(H,14,15);1H
InChI key
DWOIUCRHVWIHAH-UHFFFAOYSA-N
基因信息
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
生化/生理作用
(+)-Isomer is a selective α-adrenoceptor antagonist; (−)-isomer is an imidazoline ligand that induces insulin secretion, mediated by the blockade of ATP-sensitive potassium channels in pancreatic β cells; I1 imidazoline binding site antagonist.
(+)-Isomer is a selective α-adrenoceptor antagonist; (−)-isomer is an imidazoline ligand; I1 imidazoline binding site antagonist.
特点和优势
This compound is featured on the Imidazoline Binding Sites and Potassium Channels pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
A Szollosi et al.
British journal of pharmacology, 159(3), 669-677 (2010-02-05)
ATP-sensitive potassium channels (K(ATP) channels) in beta cells are a major target for insulinotropic drugs. Here, we studied the effects of selected stimulatory and inhibitory pharmacological agents in islets lacking K(ATP) channels. We compared insulin secretion (IS) and cytosolic calcium
T L Berridge et al.
European journal of pharmacology, 213(2), 205-212 (1992-03-24)
The effects of efaroxan (RX 821037A; 2-[2-(2-ethyl-2,3-dihydrobenzofuranyl)]-2-imidazoline HCl) at alpha 1- and alpha 2-adrenoceptors were investigated in isolated tissues, pithed rats and conscious rats. In isolated tissues, efaroxan competitively antagonised the inhibitory effects of p-aminoclonidine in the electrically stimulated (0.1
V Fagerholm et al.
British journal of pharmacology, 154(6), 1287-1296 (2008-05-22)
The imidazoline-type alpha2-adrenoceptor antagonists (+/-)-efaroxan and phentolamine increase insulin secretion and reduce blood glucose levels. It is not known whether they act by antagonizing pancreatic beta-cell alpha2-adrenoceptors or by alpha2-adrenoceptor-independent mechanisms. Many imidazolines inhibit the pancreatic beta-cell KATP channel, which
Masoomeh Sabetkasaie et al.
European journal of pain (London, England), 11(5), 535-541 (2006-08-29)
The aim of the study was to investigate the possible role of MK-801, an NMDA antagonist, in analgesia induced by rilmenidine, an imidazoline (I(1)) agonist, in mice in the formalin test. 25 microl of formalin 2.5% was injected into the
J C Chapman et al.
Diabetes, 48(12), 2349-2357 (1999-12-02)
The properties of ATP-sensitive K+ (K(ATP)) channels were explored in the electrofusion-derived, glucose-responsive, insulin-secreting cell line BRIN-BD11 using patch-clamp techniques. In intact cells, K(ATP) channels were inhibited by glucose, the sulfonylurea tolbutamide, and the imidazoline compounds efaroxan and phentolamine. Each
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